pyrazin amide

出典: meddic


UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

英文文献

  • Characterization of a novel CRAC inhibitor that potently blocks human T cell activation and effector functions.
  • Chen G1, Panicker S, Lau KY, Apparsundaram S, Patel VA, Chen SL, Soto R, Jung JK, Ravindran P, Okuhara D, Bohnert G, Che Q, Rao PE, Allard JD, Badi L, Bitter HM, Nunn PA, Narula SK, DeMartino JA.Author information 1Inflammation Discovery, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, USA. gang.chen21@gmail.comAbstractStore operated calcium entry (SOCE) downstream of T cell receptor (TCR) activation in T lymphocytes has been shown to be mediated mainly through the Calcium Release Activated Calcium (CRAC) channel. Here, we compared the effects of a novel, potent and selective CRAC current inhibitor, 2,6-Difluoro-N-{5-[4-methyl-1-(5-methyl-thiazol-2-yl)-1,2,5,6-tetrahydro-pyridin-3-yl]-pyrazin-2-yl}-benzamide (RO2959), on T cell effector functions with that of a previously reported CRAC channel inhibitor, YM-58483, and a calcineurin inhibitor Cyclosporin A (CsA). Using both electrophysiological and calcium-based fluorescence measurements, we showed that RO2959 is a potent SOCE inhibitor that blocked an IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells stably expressing human Orai1 and Stim1, as well as SOCE in human primary CD4(+) T cells triggered by either TCR stimulation or thapsigargin treatment. Furthermore, we demonstrated that RO2959 completely inhibited cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction). Lastly, we showed by gene expression array analysis that RO2959 potently blocked TCR triggered gene expression and T cell functional pathways similar to CsA and another calcineurin inhibitor FK506. Thus, both from a functional and transcriptional level, our data provide evidence that RO2959 is a novel and selective CRAC current inhibitor that potently inhibits human T cell functions.
  • Molecular immunology.Mol Immunol.2013 Jul;54(3-4):355-67. doi: 10.1016/j.molimm.2012.12.011. Epub 2013 Jan 26.
  • Store operated calcium entry (SOCE) downstream of T cell receptor (TCR) activation in T lymphocytes has been shown to be mediated mainly through the Calcium Release Activated Calcium (CRAC) channel. Here, we compared the effects of a novel, potent and selective CRAC current inhibitor, 2,6-Difluoro-N
  • PMID 23357789
  • [Development and biochemical characterization of EGFR/c-Met dual inhibitors].
  • Szokol B1, Gyulavári P2, Baska F1, Ibolya K1, Greff Z1, Szántai KC1, Zoltán O3, Peták I2, Axel U3, Vantus T2, Kéri G1, Orfi L1.Author information 1Vichem Chemie Kutató Kft.2Orvosi Vegytani, Molekuláris Biológiai és Patobiokémiai Intézet, Semmelweis Egyetem.3Max Planck Institute of Biochemistry, Department of Molecular Biology, München.AbstractThe epidermal growth factor receptor (EGFR) family has been well-known for more than ten years as the target of non-small lung carcinoma (NSCLC) which is one of the leading cause of mortality among the cancer types. The receptor tyrosine kinase inhibitors (gefitinib, erlotinib, lapatinib) which have been applied in the therapy, are not able to inhibit the progression of this disease perfectly because of resistance. It has been demonstrated that the amplification of mesenchymal-epithelial transition factor (c-Met) or secondary mutation of EGFR kinase causes the resistance against EGFR inhibitors in 18-20 percent of the cases. Clinical candidates inhibiting both of EGFR and c-Met kinases are unknown in the literature. We have developed quinoline-based inhibitors in our research project, which inhibit both kinases in submicromolar range in enzymatic assays, moreover we have demonstrated by western blot analysis that these compounds inhibit the autophosphorylation in vivo. The binding of the effective compounds was examined by in silico and docking simulations.
  • Acta pharmaceutica Hungarica.Acta Pharm Hung.2013;83(4):121-33.
  • The epidermal growth factor receptor (EGFR) family has been well-known for more than ten years as the target of non-small lung carcinoma (NSCLC) which is one of the leading cause of mortality among the cancer types. The receptor tyrosine kinase inhibitors (gefitinib, erlotinib, lapatinib) which have
  • PMID 24575658
  • Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
  • Zhan P1, Chen W, Li Z, Li X, Chen X, Tian Y, Pannecouque C, Clercq ED, Liu X.Author information 1Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong, PR China.AbstractThe present work is an extension of our ongoing efforts towards the development and identification of new molecules with anti-HIV activity which have previously led to the discovery of arylazolylthioacetanilides as highly active NNRTIs. In this article, a series of 2-2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamide derivatives were synthesized and evaluated for in vitro anti-HIV activity. Most of the tested compounds exhibited moderate activities against wild-type HIV-1. Among them, compound 6k showed significant activity against wild-type HIV-1 with an EC(50) value of 1.7μM, along with moderate activity against wild-type reverse transcriptase (RT). The preliminary structure-activity relationship (SAR) and docking calculations of this new series of compounds were also investigated, which may help designing more potent molecules.
  • Bioorganic & medicinal chemistry.Bioorg Med Chem.2012 Dec 1;20(23):6795-802. doi: 10.1016/j.bmc.2012.09.058. Epub 2012 Oct 6.
  • The present work is an extension of our ongoing efforts towards the development and identification of new molecules with anti-HIV activity which have previously led to the discovery of arylazolylthioacetanilides as highly active NNRTIs. In this article, a series of 2-2-(3-(2-chlorophenyl)pyrazin-2-y
  • PMID 23098609

関連リンク

N-pyrazin-2-ylnitrous amide - chemical information, properties, structures, articles, patents and more chemical data. Enter your search term above and find: · CAS Numbers · Molecular Formulas · Synonyms · Sites/Web Search · Suppliers
Moxifloxacin-based Regimens for Tuberculosis n engl j med 371;17 nejm.org , october 22014 3 1579 which consisted of isoniazid, rifampin, pyrazin-amide, and ethambutol for 8 weeks, followed by 18 weeks of isoniazid and rifampin ...

関連画像

Figure imgf000044_0001Figure imgf000097_0001Figure imgf000046_0001Figure imgf000071_0001Spectrum of 38750-39-9 (7H-Dibenzo[de,g Figure imgf000020_0002


★リンクテーブル★
関連記事amide」「amid

amide」

  [★]

アミド

WordNet   license wordnet

「any organic compound containing the group -CONH2」

PrepTutorEJDIC   license prepejdic

「アミド[基化物]」


amid」

  [★]

  • 真ん中に

PrepTutorEJDIC   license prepejdic

「…の中に;…のまっさい中に」




★コメント★

[メモ入力エリア]
※コメント5000文字まで
ニックネーム:
コメント:




表示
個人用ツール


  meddic.jp

リンク
連絡